Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0000648 |
| PMID | 12467226 |
| Assay Used | In Vitro Inhibition of Kinase Activity and In Vitro Growth Inhibition assay |
| Experimently Validated | Yes |
| EGFR (IC50) | 10.8 +/- 0.53 nM |
| HER2 (IC50) | 9.2 ± 0.75 nM |
| HER4 (IC50) | 367 ± 4.2 nM |
| Mutant L858R (IC50) | - |
| Mutant T790M (IC50) | - |
| Double Mutant (IC50) | - |
| Average ERBB2 and ERBB1 (IC50) | - |
| Inhibition EGFR (%) | - |
| Inhibitory Concentration | - |
| Inhibition HER2 (%) | - |
| Inhibitory Concentration | - |
| Ki (EGFR) | - |
| Ki (HER2) | - |
| Ki (HER4) | - |
| Kd (EGFR) | - |
| Kd (L858R) | - |
| Kd (T790M) | - |
| Kd (L858R/T790M) | - |
| Kd (Other mutation) | - |
| Note | The paper decribes the reversible Epidermal Growth Factor Receptor/ErbB-2 Tyrosine Kinase Inhibitor, GW2016, on the Growth of Human Normal and Tumor-derived Cell Lines in Vitro and in Vivo. |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | A431 | - | 160 ±30 nM | - | - | - | - | - | - | - | - | |||
| 2 | BT474 | - | 100 ±30 nM | - | - | - | - | - | - | - | - | |||
| 3 | CaLu3 | - | 130 ±30 nM | - | - | - | - | - | - | - | - | |||
| 4 | HB4a | - | 9100 ±800 nM | - | - | - | - | - | - | - | - | |||
| 5 | HB4a | - | 210 ±30 nM | - | - | - | - | - | - | - | - | |||
| 6 | HFF | - | 12000 ± 1400 nM | - | - | - | - | - | - | - | - | |||
| 7 | HN5 | - | 120 ±30 nM | - | - | - | - | - | - | - | - | |||
| 8 | MCF-7 | - | 4000 ± 100 nM | - | - | - | - | - | - | - | - | |||
| 9 | N87 | - | 90 ±20 nM | - | - | - | - | - | - | - | - | |||
| 10 | T47D | - | 3000 ±200 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | Yes |
| Wild type | Yes |
| Mutant | - |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |